Rapid Construction of 18F-Triazolyl-tetrazines through the Click Reaction.
J Org Chem
; 2024 Jun 14.
Article
em En
| MEDLINE
| ID: mdl-38875503
ABSTRACT
Due to the fast reaction rate, 18F-labeled tetrazines have been widely applied in positron emission tomography (PET) imaging in cancer research and drug discovery. In this work, several functional 18F-triazolyl-tetrazines were rapidly obtained through an optimized copper-catalyzed alkyene-azide cycloaddition reaction system in >99% radiochemical conversions. Notably, the commonly used 18F-labeled azides were isolated through cartridges and directly used for cycloadditions, which greatly simplified the labeling procedure. The assembled triazolyl-tetrazines demonstrated high in vitro stability and reaction kinetics, exhibiting considerable potential for the development of PET agents.
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MEDLINE
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En
Ano de publicação:
2024
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Article
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